Geisslinger G, Stock K P, Bach G L, Loew D, Brune K
Department of Pharmacology, University of Erlangen, FRG.
Agents Actions. 1989 Jun;27(3-4):455-7. doi: 10.1007/BF01972851.
Ibuprofen (IBU) is a non-steroidal anti-inflammatory drug exhibiting optical isomerism. Only the racemate is in clinical use. In in vitro studies it has been demonstrated that only the S(+)-enantiomer inhibits the PG synthetase system. Nevertheless, it is widely believed that the sole use of the active isomer does not comprise any advantages since the inactive isomer is converted within the human body. In a triple cross-over study (300 mg S(+), 300 mg R(-), 600 mg racemic IBU; n = 8), we could show that the converted R(-)-IBU after racemate administration provides for only one third of the AUC of S(+)-IBU obtained after S(+)-application. Highest S(+)-peak plasma levels were reached after S(+)-IBU, lower ones after racemate. We, therefore, studied 4 patients with classical rheumatoid arthritis treated with 2-3 doses of 500 mg of S(+)-IBU/day over a two week period. Significant clinical recovery (Ritchie-index p less than 0.01; analogue scale pain p less than 0.05, motion p less than 0.01) was reached after one week. The results indicate that a reduction of dose and of metabolic load is possible if the S(+)-enantiomer is administrated.
布洛芬（IBU）是一种具有光学异构性的非甾体抗炎药。临床上仅使用其消旋体。体外研究表明，只有S(+)-对映体能够抑制PG合成酶系统。然而，人们普遍认为单独使用活性异构体并无任何优势，因为非活性异构体在人体内会发生转化。在一项三交叉研究（300mg S(+)、300mg R(-)、600mg消旋布洛芬；n = 8）中，我们发现消旋体给药后转化生成的R(-)-布洛芬的AUC仅为S(+)-布洛芬给药后所得AUC的三分之一。S(+)-布洛芬给药后达到的S(+)-血浆峰值水平最高，消旋体给药后的峰值水平较低。因此，我们对4例经典类风湿关节炎患者进行了研究，在两周内给予他们2 - 3剂每日500mg的S(+)-布洛芬。一周后患者实现了显著的临床康复（里奇指数p < 0.01；视觉模拟评分法疼痛p < 0.05，活动度p < 0.01）。结果表明，给予S(+)-对映体时可以降低剂量和代谢负荷。
